Altair Therapeutics Reports Successful Phase I Study of Inhaled AIR645

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Mon Sep 14, 2009 9:00am EDT

Data Presented at European Respiratory Society Annual Congress Shows Potential
Asthma Treatment to be Safe and Well-Tolerated
SAN DIEGO & VIENNA--(Business Wire)--
Altair Therapeutics, Inc., a privately-held, biopharmaceutical company
developing novel therapeutics for respiratory diseases, today announced positive
results from a phase I multiple dose safety and pharmacokinetic study of its
lead product,once-weekly inhaled AIR645 in healthy adults and mild asthmatics.
The results were presented today by Dr. Michael Hodges, M.D., Chief Medical
Officer for Altair Therapeutics at the European Respiratory Society Annual
Congress in Vienna. 

AIR645 isa non-steroidal dual inhibitor of cellular responses to interleukin
(IL)-4 and IL-13. These pro-inflammatory cytokines orchestrate the adaptive
immune response to inhaled allergens and viruses and the development of chronic
inflammation in asthma, rhinitis and other respiratory disorders. The
randomized, placebo-controlled trial evaluated the safety, tolerability,
bioavailability and pharmacodynamic activity of nebulized AIR645 at multiple
dose levels in 32 healthy adult subjects (0.3, three, 10, and 20 mg/dose) and
eight mild asthma subjects (20mg/dose). Subjects were sequentially randomized
(six active: two placebo) and received six doses on study days one, three, five,
eight, 15 and 22. 

AIR645 was safe and well tolerated. No dose-limiting toxicities or safety
signals were detected in this clinical study. Adverse effects were mostly mild
and none were considered severe, significant, or serious and no subjects were
discontinued due to adverse events. 

AIR645 exposure in sputum was found to be dose-dependent, and no accumulation of
drug was evident. AIR645 half-life in sputum was calculated to be approximately
5 days. AIR645 concentration was >1000-fold higher in sputum than in plasma,
indicating very low systemic bioavailability of the drug. 

Following repeated inhalation of AIR645 evidence of anti-inflammatory biomarker
activity was seen in subjects with mild asthma (those that had baseline
elevations of biomarkers), including reductions in serum total IgE, sputum
eosinophils or level of 15-HETE in sputum. 

"The AIR645 pharmacokinetics and distribution profile demonstrated in this study
are consistent with preclinical findings and support effective once-weekly or
once-daily administration of this 2'-O-methoxyethyl modified oligonucleotide in
humans," commented Susan Gregory, Ph.D., Chief Scientific Officer for Altair
Therapeutics. "We believe that IL-4Rα inhibition can prevent and retard asthma
pathogenesis and will prove to be a valuable therapeutic approach to asthma,
chronic obstructive pulmonary disease and other respiratory disorders." 

"The safety and PK data from this study underscore the potential of AIR645 as a
new, safe and effective non-steroidal anti-inflammatory control medication for
asthma," said Dr. Hodges. "The dosing flexibility afforded by the projected long
tissue half-life of this drug opens the door to improved patient compliance
using a once-daily inhaler or using once-weekly nebulized formulations." 

"AIR645 is based upon a proprietary anti-sense molecular design - termed `MOE
gapmer` - that greatly improves potency, stability, safety and tolerability in
vivo," said Joel F. Martin, Ph.D., President and CEO of Altair Therapeutics.
"AIR645 is the first such MOE gapmer oligonucleotide to be administered by
inhalation in man and has now demonstrated favorable safety and pharmacokinetic
profiles. The results are particularly remarkable because AIR645, a low
cost-of-goods drug, inhibits a target that, to date, has been approachable only
by expensive biologics." 

About AIR645

AIR645 is a dual inhibitor of IL-4 and IL-13, pro-inflammatory cytokines which
are implicated in the pathogenesis of asthma, allergic rhinitis and other
inflammatory disorders. AIR645 is a 2'-O-methoxyethyl second-generation
antisense drug targeting the mRNA that encodes the alpha subunit of the human
IL-4 receptor (IL-4Rα). IL-4Rα is the signaling chain that is shared by the IL-4
and IL-13 receptors and is required for cellular responses to IL-4 and IL-13.
AIR645 has the potential for less frequent administration with improved local
and systemic safety. AIR645 was discovered by Isis Pharmaceuticals, Inc.
(NASDAQ: ISIS) and licensed to Altair Therapeutics. 

About Altair Therapeutics

Based in San Diego, Altair Therapeutics, Inc. is a privately-held
biopharmaceutical company developing novel therapeutics to treat human
respiratory diseases. Altair Therapeutics` lead product is AIR645, the first in
a new class of inhaled drugs that incorporate proprietary, second-generation
antisense chemistry. www.altairthera.com





College Hill Life Sciences for Altair Therapeutics
Erik Clausen or Kena Hudson, 415-230-5385
Erik.Clausen@collegehill.com
Kena.Hudson@collegehill.com

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